Synthesis, Cytotoxicity and Antitumor Activity of Platinum(II) Complexes of Cyclopentanecarboxylic Acid Hydrazide
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Daniel Kushev
Abstract
New platinum(II) complexes of cyclopentanecarboxylic acid hydrazide (cpcah) were prepared, characterized by elemental analysis, IR and 1H NMR spectra, and evaluated for in vitro cytotoxicity in Friend leukemia (FL) and A2780 ovarian tumor cells, induction of apoptosis in FL cells, as well as for in vivo antitumor activity toward murine L1210 leukemia and Lewis lung carcinoma. The spectral analyses indicated a cissquare planar structure of the complexes with hydrazide ligand coordinated via the NH2 group. The compounds exerted significantly lower in vitro and in vivo toxicities as compared with those of cisplatin (cis-diamminedichloroplatinum(II), DDP). On the other hand, the complex [Pt(NH3)(cpcah)Cl2] exhibited antitumor activity against L1210 leukemia in mice comparable to that of cisplatin, resulting at a dose of 42 mg/kg (administered 3 times) in a T/C (mean survival time) of 280%. This compound displayed an in vitro macromolecular synthesis inhibition pattern similar to that of DDP. At concentrations close to the cytostatic ones (10–20 μM) this complex, as well as DDP, was able to induce apoptosis in FL cells as shown by neutral comet assay and morphological analysis. We concluded that there is a correlation between the ability of platinum complexes to induce apoptosis and their antitumor activity.
Copyright © 1999 by Walter de Gruyter GmbH & Co. KG
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- High Activity of the Calcineurin A Subunit with a V314 Deletion
- Synthesis, Cytotoxicity and Antitumor Activity of Platinum(II) Complexes of Cyclopentanecarboxylic Acid Hydrazide
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- Mass Spectrometric Characterisation of Post-Translational Modification and Genetic Variation in Human Tetranectin
- Complete Amino Acid Sequence Determination of the Major Allergen of Peach (Prunus persica) Pru p1
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- An Evaluation of Techniques for the Extraction and Amplification of DNA from Naturally Shed Hairs
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